PE20091384A1 - THENOPYRIMIDINE AND PYRAZOLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF KINASE MTOR AND KINASE P13 - Google Patents

THENOPYRIMIDINE AND PYRAZOLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF KINASE MTOR AND KINASE P13

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Publication number
PE20091384A1
PE20091384A1 PE2008001780A PE2008001780A PE20091384A1 PE 20091384 A1 PE20091384 A1 PE 20091384A1 PE 2008001780 A PE2008001780 A PE 2008001780A PE 2008001780 A PE2008001780 A PE 2008001780A PE 20091384 A1 PE20091384 A1 PE 20091384A1
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Prior art keywords
kinase
halo
oxa
pyrimidin
oct
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PE2008001780A
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Spanish (es)
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Arie Zask
Joshua Aaron Kaplan
Jeroen Cunera Verheijen
Kevin J Curran
David James Richard
Semiramis Ayral-Kaloustian
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Wyeth Corp
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Publication of PE20091384A1 publication Critical patent/PE20091384A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
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  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
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  • Hematology (AREA)
  • Cardiology (AREA)
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  • Endocrinology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
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  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

REFERIDA A COMPUESTOS DERIVADOS DE TIENOPIRIMIDINA Y PIRAZOLOPIRIMIDINA DE FORMULAS (Ia) Y (IIa), DONDE Het ES UN HETEROBICICLILO DE 5 A 10 MIEMBROS QUE CONTIENE POR LO MENOS UN ATOMO DE O Y N; Y OPCIONALMENTE HETEROATOMOS ADICIONALES DE O, S Y N; R20 ES OH, HALO, ALCOXI(C1-C2), ENTRE OTROS; R1 ES HALO, ALQUILO(C1-C6), ENTRE OTROS; R2 ES H, HALO, ACILO(C1-C8), ENTRE OTROS; R3 ES H, ALQUILO(C1-C6), ENTRE OTROS; R8 ES H, HALO, ALQUILO(C1-C6), ENTRE OTROS; Ar ES FENILO, NAFTILO, ENTRE OTROS; t ES DE 0 A 16; m ES DE 0 A 4; r ES 0 O 1. SON COMPUESTOS PREFERIDOS: 3-[4-(8-OXA-3-AZABICICLO[3.2.1]OCT-3-1L)-1-FENIL-1H-PIRAZOLO[3,4-d]PIRIMIDIN-6-IL]FENOL, 1-METIL-3-{4-[4-(8-OXA-3-AZABICILO[3.2.1]OCT-3-IL)-1-(2,2,2-TRIFLUOROETIL)-1H-PIRAZOLO[3,4-d]PIRIMIDIN-6-IL]FENIL}UREA, {4-[4-(8-OXA-3-AZABICICLO[3.2.1]OCT-3-IL)-1-(2,2,2-TRIFLUOROETIL)-1H-PIRAZOLO[2,3-d]PIRIMIDIN-6-IL]FENIL}CARBAMATO DE METILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE QUINASA mTOR Y DE QUINASA PI3K, SIENDO UTILES PARA EL TRATAMIENTO DE TRASTORNOS OSEOS, CANCER DE PROSTATA, ANGIOGENIA, ENTRE OTROSREFERRING TO COMPOUNDS DERIVED FROM THENOPYRIMIDINE AND PYRAZOLOPYRIMIDINE FROM FORMULAS (Ia) AND (IIa), WHERE Het IS A HETEROBICYCLYL OF 5 TO 10 MEMBERS THAT CONTAINS AT LEAST ONE ATOM OF O AND N; AND OPTIONALLY ADDITIONAL O, S AND N HETEROATOMS; R20 IS OH, HALO, ALCOXY (C1-C2), AMONG OTHERS; R1 IS HALO, ALKYL (C1-C6), AMONG OTHERS; R2 IS H, HALO, ACILO (C1-C8), AMONG OTHERS; R3 IS H, (C1-C6) ALKYL, AMONG OTHERS; R8 IS H, HALO, (C1-C6) ALKYL, AMONG OTHERS; Ar IS PHENYLUS, NAFTHYLUS, AMONG OTHERS; t IS 0 TO 16; m IS 0 TO 4; r IS 0 O 1. PREFERRED COMPOUNDS ARE: 3- [4- (8-OXA-3-AZABICYCLE [3.2.1] OCT-3-1L) -1-PHENYL-1H-PYRAZOLE [3,4-d] PYRIMIDIN -6-IL] PHENOL, 1-METHYL-3- {4- [4- (8-OXA-3-AZABYCLO [3.2.1] OCT-3-IL) -1- (2,2,2-TRIFLUOROETHYL) -1H-PYRAZOLO [3,4-d] PYRIMIDIN-6-IL] PHENYL} UREA, {4- [4- (8-OXA-3-AZABICYCLO [3.2.1] OCT-3-IL) -1- ( 2,2,2-TRIFLUOROETHYL) -1H-PYRAZOLO [2,3-d] PYRIMIDIN-6-IL] PHENYL} METHYL CARBAMATE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PREPARATION PROCEDURE. SUCH COMPOUNDS ARE INHIBITORS OF mTOR KINASE AND PI3K KINASE, BEING USEFUL FOR THE TREATMENT OF BONE DISORDERS, PROSTATE CANCER, ANGIOGENIA, AMONG OTHERS

PE2008001780A 2007-10-16 2008-10-16 THENOPYRIMIDINE AND PYRAZOLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF KINASE MTOR AND KINASE P13 PE20091384A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US98033207P 2007-10-16 2007-10-16
US2759508P 2008-02-11 2008-02-11

Publications (1)

Publication Number Publication Date
PE20091384A1 true PE20091384A1 (en) 2009-09-09

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PE2008001780A PE20091384A1 (en) 2007-10-16 2008-10-16 THENOPYRIMIDINE AND PYRAZOLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF KINASE MTOR AND KINASE P13

Country Status (26)

Country Link
US (1) US8129371B2 (en)
EP (1) EP2212333A1 (en)
JP (1) JP2011500702A (en)
KR (1) KR20100083170A (en)
CN (1) CN101883774A (en)
AP (1) AP2010005234A0 (en)
AR (1) AR068898A1 (en)
AU (1) AU2008312631A1 (en)
BR (1) BRPI0817681A2 (en)
CA (1) CA2702838A1 (en)
CL (1) CL2008003061A1 (en)
CO (1) CO6321257A2 (en)
CR (1) CR11373A (en)
DO (1) DOP2010000118A (en)
EA (1) EA201000484A1 (en)
EC (1) ECSP10010112A (en)
IL (1) IL205109A0 (en)
MA (1) MA31884B1 (en)
MX (1) MX2010004260A (en)
NI (1) NI201000060A (en)
PA (1) PA8799101A1 (en)
PE (1) PE20091384A1 (en)
TN (1) TN2010000171A1 (en)
TW (1) TW200922593A (en)
WO (1) WO2009052145A1 (en)
ZA (1) ZA201003430B (en)

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